Shin Jai Moo, Sachs George
Department of Physiology, David Geffen School of Medicine, University of California at Los Angeles, and VA Greater Los Angeles Healthcare System, Los Angeles, CA 90073.
Expert Rev Clin Pharmacol. 2009 Sep;2(5):461-468. doi: 10.1586/ecp.09.33.
Proton pump inhibitors (PPIs) are acid-activated prodrugs which covalently bind to the gastric H,K-ATPase on its luminal surface. Only active pumps can be inhibited. The short plasma residence time of current PPIs prevents inhibition of pumps synthesized or activated after the PPI has disappeared, limiting the degree of acid inhibition even with BID administration. PPIs with a longer residence time should improve acid control. Various K(+) competitive inhibitors of the pump are being developed (APAs or PCABs), with the advantage of complete inhibition of acid secretion independent of pump activity. Early data on these suggest that twice a day administration would improve acid control compared to PPIs.
质子泵抑制剂（PPIs）是酸激活的前体药物，可与胃腔表面的胃H，K - ATP酶共价结合。只有活性泵才能被抑制。目前PPIs的血浆停留时间较短，这使得在PPI消失后合成或激活的泵无法被抑制，即使每日两次给药也限制了胃酸抑制程度。停留时间更长的PPIs应该能改善胃酸控制。目前正在研发各种钾离子竞争性泵抑制剂（APAs或PCABs），其优点是能完全抑制胃酸分泌，而与泵的活性无关。关于这些药物的早期数据表明，与PPIs相比，每日两次给药能改善胃酸控制。
